Tianjin Medical Journal ›› 2018, Vol. 46 ›› Issue (7): 765-770.doi: 10.11958/20171266

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Clinical research progress of proprotein convertase subtilisin/kexin type 9 inhibitors

CUI Li, LI Guang-ping△   

  1. Tianjin Key Laboratory of Ionic-Molecular Function of Cardiovascular Disease, Department of Cardiology, Tianjin Institute of Cardiology, the Second Hospital of Tianjin Medical University, Tianjin 300211, China △Corresponding Author and Revisor E-mail: tic_tjcardiol@126.com
  • Received:2017-11-14 Revised:2018-03-16 Published:2018-07-15 Online:2018-07-15

Abstract: Proprotein convertase subtilisin / kexin type 9 (PCSK9) inhibitors can reduce the low density lipoprotein cholesterol (LDL-C) level in circulatory system by blocking PCSK9-low density lipoprotein receptor (LDLR) pathway to mediate the degradation of LDLR. At present, PCSK9 inhibitors have become the focus of cardiovascular lipid-lowering therapy. A variety of PCSK9 inhibitors have entered the clinical trial stage. This paper mainly reviews the molecular structure and mechanism of PCSK9, the classification of PCSK9 inhibitors, and recent clinical study of the monoclonal antibodies of PCSK9 inhibitors in order to evaluate the effectiveness and long-term safety of cardiovascular risk reduction.

Key words: lipoproteins, LDL, antibodies, monoclonal, proprotein convertase subtilisin/kexin type 9, review